| Bioactivity | MtInhA-IN-1 is a selective and orally active Mycobacterium tuberculosis NADH-dependent enoyl-acyl carrier protein reductase (MtInhA) inhibitor with an IC50 of 0.23 μM. MtInhA-IN-1 potently against M. tuberculosis H37Rv strain with a MIC value of 0.4 μM[1]. |
| Target | IC50: 0.23 μM (Mycobacterium tuberculosis NADH-dependent enoyl-acyl carrier protein reductase (MtInhA))MIC: 0.4 μM (M. tuberculosis H37Rv strain), 0.1 μM (M. tuberculosis strains PT2), 0.2 μM (M. tuberculosis strains PT12), and 0.1 μM (M. tuberculosis strains PT20) |
| Invitro | MtInhA-IN-1 (compound 19k) 显示出对一组多重耐药结核分枝杆菌菌株、结核分枝杆菌菌株 PT2、PT12 和 PT20 的抑制活性。对 PT2、PT12 和 PT20 的 MIC 值分别为 0.1 μM、0.2 μM 和 0.1 μM。此外，MtInhA-IN-1 对 HepG2 和 Vero 细胞的细胞毒性较低[1]。 |
| In Vivo | MtInhA-IN-1 (compound 19k; 300-450 μM/kg; p.o; daily; for 14 days）在小鼠结核病模型中表现出抑菌作用[1]。 Animal Model: |
| Name | MtInhA-IN-1 |
| Formula | C21H22BrN3 |
| Molar Mass | 396.32 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Josiane Delgado Paz, et al. Novel 4-aminoquinolines: Synthesis, inhibition of the Mycobacterium tuberculosis enoyl-acyl carrier protein reductase, antitubercular activity, SAR, and preclinical evaluation. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114908. |